Abstract
The synthesis of β3-adrenergic receptor agonists A and B with radiolabeled amide fragment, required for drug disposition studies, was accomplished based on initial formation of 2-(4-(2-amino-2-methylpropyl)phenoxy)-5-[14C]-cyanopyridine by the reaction of 2-bromo-5-iodopyridine with para-substituted phenol, and following cyanation of aromatic iodide with potassium cyanide-[14C]. After the coupling of the resulted amine with glycidyl derivatives of 4-hydroxyindole and 4-hydroxycarbazole, the corresponding nitriles were hydrolyzed with basic hydrogen peroxide to obtain target amides A and B. Copyright © 2006 John Wiley & Sons, Ltd.
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